Novel Furin Inhibitors with Potent Anti‐infectious Activity

New peptidomimetic furin inhibitors with unnatural amino acid residues in the P3 position were synthesized. The most potent compound 4‐guanidinomethyl‐phenylacteyl‐Arg‐Tle‐Arg‐4‐amidinobenzylamide (MI‐1148) inhibits furin with a K_i value of 5.5 pM . The derivatives also strongly inhibit PC1/3, whereas PC2 is less affected. Selected inhibitors were tested in cell culture for antibacterial and antiviral activity against infectious agents known to be dependent on furin activity. A significant protective effect against anthrax and diphtheria toxin was observed in the presence of the furin inhibitors. Furthermore, the spread of the highly pathogenic H5N1 and H7N1 avian influenza viruses and propagation of canine distemper virus was strongly inhibited. Inhibitor MI‐1148 was crystallized in complex with human furin. Its N‐terminal guanidinomethyl group in the para position of the P5 phenyl ring occupies the same position as that found previously for a structurally related inhibitor containing this substitution in the meta position, thereby maintaining all of the important P5 interactions. Our results confirm that the inhibition of furin is a promising strategy for a short‐term treatment of acute infectious diseases.     

Thermal Stability,Optical Transmittance,and Refractive Index Dispersion of La2O3–Nb2O5–Al2O3 Glasses

La₂O₃–Nb₂O₅–Al₂O₃ high‐refractive‐index glasses were fabricated by containerless processing, and the glass‐forming region was determined. The thermal stability, density, optical transmittance, and the refractive index dispersion of these glasses were investigated. All the glasses were colorless and transparent in the visible to near infrared (NIR) region and had high refractive index with low wavelength dispersion. Some of these glasses were found to have significantly high glass‐forming ability. These results indicate that the ternary glasses are suitable for optical applications in the visible to NIR region. The effects of the substitution of Al₂O₃ for Nb₂O₅ on optical properties were discussed on the basis of the Drude–Voigt equation. It was suggested that the substitution of Al₂O₃ for Nb₂O₅ increased the molecular density and suppressed a decrease in the refractive index, even when both the average oscillator strength and inherent absorption wavelength decreased in La₂O₃–Nb₂O₅–Al₂O₃ glasses. These results are helpful for designing new optical glasses controlled to have a higher refractive index and lower wavelength dispersion.     

Reaction Pathways in the Synthesis of Photorefractive gamma-Bi12MO20 (M = Si, Ge, or Ti)

Reaction pathways in the synthesis of three photorefractive silicates—γ-Bi₁₂ SiO₂₀ (BSO), γ-Bi₁₂ GeO₂₀ (BGO), and gamma-Bi₁₂ TiO₂₀ (BTO)—were systematically investigated. The main results were as follows: (i) all the reactions of the form 6Bi₂O₃+ MO₂→> γ-Bi₁₂ MO₂₀ (SR1 for M = Si, SR2 for M = Ge, SR3 for M = Ti) in the solid state seemed to be diffusion-controlled processes and were affected by both temperature and time, where the reaction temperature increases in the order SR1 < SR2 < SR3; (ii) the metastable phases Bi₂ SiO₅ (tetragonal) in reaction SR1, Bi₂ GeO₅ (orthorhombic) in reaction SR2, Bi₄ Ti₃ O₁₂ (orthorhombic) in reaction SR3 may be formed and seemed to greatly accelerate the above-mentioned solid-state reaction processes; and (iii) for a continuous heating process, pure γ-Bi₁₂ SiO₂₀ and γ-Bi₁₂ GeO₂₀ could be produced before melting, whereas pure γ-Bi₁₂ TiO₂0 could not be produced, even if all the mixed phases had melted.     

In Situ Observation of Phase Separation of a Barium Borate Melt in a Stable Immiscibility Region under Microgravity

The precipitation of droplets was directly observed on a BaO–B₂O₃ melt in a drop shaft experiment. This is the first time that precipitation of droplets has been observed in a 4.5 s drop test. The melt film of 4BaOz96B₂O₃ (mol%) held on a platinum wire loop was heated above the critical tem-perature to produce uniformity and was cooled down to the phase separation temperature range. Phase separation of the melt was observed directly with a video camera. The IR image of the melt was simultaneously detected with a CCD array and was converted into a two-dimensional thermograph.     

Compatibilization of recycled poly(ethylene terephthalate) and polypropylene blends: Effect of polypropylene molecular weight on homogeneity and compatibility

The effectiveness of compatibilizers in enhancing the dispersion of polypropylene (PP) at various molecular weights in recycled polyethylene terephthalate (RPET) was elucidated. The idea of incorporating PP of different molecular weights evolved from the intention of simultaneously recycling the PET bottles together with the PP‐based bottle caps, which are often of low molecular weight (M_w). Three grades of PP with known molecular weights were blended with RPET at various loadings of compatibilizers. Morphological analyses suggest that the dispersion of the PP particles was more homogeneous, and the average particle size was smaller when low M_w PP was incorporated. This indicates that the interaction between the compatibilizer and PP particles was more intense with the presence of a large number but shorter PP molecular chains. Moreover, specimens containing low M_w PP were found to remain homogeneous regardless of compatibilizer and PP content in the RPET/PP blends. The homogeneity of the blends significantly affected their mechanical performance as well. Higher stiffness, yield strength, deformability, and toughness were observed when low M_w PP was incorporated, regardless of PP and compatibilizer loadings. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

Supercritical fluid extraction of bacterial and archaeal lipid biomarkers from anaerobically digested sludge

Supercritical fluid extraction (SFE) was used in the analysis of bacterial respiratory quinone (RQ), bacterial phospholipid fatty acid (PLFA), and archaeal phospholipid ether lipid (PLEL) from anaerobically digested sludge. Bacterial RQ were determined using ultra performance liquid chromatography (UPLC). Determination of bacterial PLFA and archaeal PLEL was simultaneously performed using gas chromatography-mass spectrometry (GC-MS). The effects of pressure, temperature, and modifier concentration on the total amounts of RQ, PLFA, and PLEL were investigated by 23 experiments with five settings chosen for each variable. The optimal extraction conditions that were obtained through a multiple-response optimization included a pressure of 23.6 MPa, temperature of 77.6 °C, and 10.6% (v/v) of methanol as the modifier. Thirty nine components of microbial lipid biomarkers were identified in the anaerobically digested sludge. Overall, the SFE method proved to be more effective, rapid, and quantitative for simultaneously extracting bacterial and archaeal lipid biomarkers, compared to conventional organic solvent extraction. This work shows the potential application of SFE as a routine method for the comprehensive analysis of microbial community structures in environmental assessments using the lipid biomarkers profile.     

采用MAMMOS技术的高密度光记录

MAMMOS(Magnetic Amplifying Magneto－ Optical System:磁畴扩大磁光系统 )是实现高密度磁光盘的有效方法。不仅能得到不依赖于磁畴长度的较大的读出信号振幅,而且还能实现超出光学系统衍射极限的分辨率。过去,为实现磁畴的复印与扩大,要对记录膜面施加垂直方向的外部磁场。而现在得知,同时施加垂直磁场和水平方向的磁场,可大幅度地提高微小磁畴的读出特性。确认采用施加水平磁场的方法,在λ =635 nm, NA=0.55的条件下, 0.15μ m的连续磁畴也能获得 BER=2× 10－ 4的读出效果。     

Phase structure in the blend of atactic poly(vinyl alcohol) with atactic poly(vinyl alcohol‐block‐vinyl acetate)

An almost fully saponified atactic poly(vinyl alcohol) and an atactic poly(vinyl alcohol‐block‐vinyl acetate) of which degree of saponification is 89 mol % were blended by a solution casting method. The phase structure of the blend film was analyzed by optical microscopy, ¹³C‐NMR, and differential scanning calorimetry. The most remarkable structure of the blend was composed of cylindrical domains penetrating the film. The swelling behavior of the blend films was also investigated in the dimethylsulfoxide and water mixed solvents to find differences in solubility and diffusion behavior between the matrix and the domain. The cylindrical domains could be selectively dissolved away in water and the film became porous. We tried to change the size of the cylindrical domain with various film preparation conditions. This aimed to turn the film into the useful filter membrane. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 86: 1807–1815, 2002